Udenafil

Catalog No.S6433

Udenafil Chemical Structure

Molecular Weight(MW): 516.66

Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.

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Biological Activity

Description Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.
Targets
PDE5 [1]
(Cell-free assay)
PDE3 [1]
(Cell-free assay)
PDE6 [1]
(Cell-free assay)
PDE2 [1]
(Cell-free assay)
8.25 nM 52 nM 53.3 nM 101 nM
In vitro

The inhibitory effect of udenafil on PDE5 is about 150-fold greater than that on PDE1 (selectivity ratio of 149). PDE11 selectivity of udenafil (selectivity ratio of 96) is relatively high, indicating a very low probability of inhibition of PDE11 at therapeutic doses of udenafil. The IC50 values for PDE2, PDE3, and PDE6 of udenafil are 101±15.1 nM, 52.0±3.53 nM, and 53.3±2.47 nM respectively[1].

In vivo

Udenafil is rapidly absorbed, reaching peak plasma concentrations at 0.8-1.3 h, then declining monoexponentially with a terminal half-life (T1/2) between 7.3 and 12.1 hours, giving it the unique pharmacokinetics of both relatively rapid onset and long duration. Udenafil has also been shown in preclinical studies to have potent erectogenic properties in rats and rabbits with a broad safety margin[2]. Absolute oral bioavailability of udenafil is only 38% in rats. This low oral bioavailability of udenafil appears to be mainly due to a considerable intestinal first-pass effect[1].

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (193.55 mM)
Ethanol 25 mg/mL (48.38 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 516.66
Formula

C25H36N6O4S

CAS No. 268203-93-6
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID